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Target
Tyrosine-protein kinase JAK2 [532-1132]
Ligand
BDBM387828
Substrate
n/a
Meas. Tech.
Enzymatic Inhibition Assay
IC50
1.60±n/a nM
Citation
 Kreutter, KD; Leonard, K; Rizzolio, MC; Smith, RC; Tichenor, MS; Wang, A Small molecule inhibitors of the JAK family of kinases US Patent  US10487083 Publication Date 11/26/2019 
Target
Name:
Tyrosine-protein kinase JAK2 [532-1132]
Synonyms:
JAK2 | JAK2 (aa 532-1132) | JAK2_HUMAN
Type:
Protein
Mol. Mass.:
69777.30
Organism:
Homo sapiens (Human)
Description:
O60674[532-1132]
Residue:
601
Sequence:
MNQMVFHKIRNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASMMSKLSHKHLVLNYGVCVCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWAMHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVPPECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAELANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRDPTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIEILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIELLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG
  
Inhibitor
Name:
BDBM387828
Synonyms:
2-(1-((1r,4r)-4-(Cyanomethyl)cyclohexyl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-N-(1H-pyrazol-3-yl)acetamide | US10294226, Compound Ex. 11 | US10487083, Example 11 | US10981911, Example 74 | US11059823, Example 11
Type:
Small organic molecule
Emp. Form.:
C21H22N8O
Mol. Mass.:
402.4524
SMILES:
O=C(Cc1nc2cnc3[nH]ccc3c2n1[C@H]1CC[C@H](CC#N)CC1)Nc1cc[nH]n1 |r,wU:18.21,wD:15.17,(-3.92,.17,;-3.15,1.5,;-1.61,1.5,;-.84,.17,;-1.46,-1.24,;-.32,-2.27,;-.32,-3.81,;1.01,-4.58,;2.35,-3.81,;3.81,-4.29,;4.72,-3.04,;3.81,-1.8,;2.35,-2.27,;1.01,-1.5,;.69,0,;1.72,1.15,;3.23,.83,;4.26,1.97,;3.78,3.44,;4.82,4.58,;6.32,4.26,;7.83,3.94,;2.28,3.76,;1.25,2.61,;-3.92,2.83,;-5.46,2.83,;-6.36,4.08,;-7.83,3.6,;-7.83,2.06,;-6.36,1.59,)|
Structure:
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